This invention relates to a process for the synthesis and method of use of an effective amount of a 3-hydroxy-3-methylbutyrate (HMB) amino acid salt for the regulation athletic function in humans. HMB synthesis traditionally has utilized many forms ranging from free acid, salt, ester, and lactone. HMB mineral salts have been the preferred form, which may consist of a sodium salt, a potassium salt, a magnesium salt, a chromium salt, and most preferably a calcium salt. This is most likely due to the fact that the mineral salts are thought to produce the most water soluble forms thereby possessing the most orally bioavailable forms. Although we purpose for the first time that the process for the synthesis and use of a HMB amino acid salt is novel, unobvious, and superior due to enhanced absorption, bioavailability and function.
HMB is a product of leucine metabolism. Leucine metabolism begins with the transanimation to the keto acid alpha-ketoisocaporate (KIC) which is then oxidized to HMB by KIC-dioxygenase. KIC continues to form ketones while HMB is utilized as a precursor to cholesterol. HMB enters the cytosol of liver and muscle and is converted to beta-hydroxy-beta-methylglutarate-Co-A (HMG-CoA), which is a precursor to cholesterol metabolism.
HMB has been patented for number of useful applications. For instance, U.S. Pat. No. 4,992,470 by Nissen demonstrates a method for enhancing immune response in mammals. U.S. Pat. No. 5,028,440 by Nissen describes a method for increasing lean tissue in animals. U.S. Pat. No. 5,348,979 by Nissen demonstrates a method for promoting nitrogen retention in humans. U.S. Pat. No. 5,360,613 by Nissen further demonstrates a method for reducing blood levels of total cholesterol and low-density lipoprotein cholesterol. More recently U.S. Pat. No. 6,392,092 by Mycoy et al. describes a process for the manufacturing of HMB salts in commercially viable amounts.
HMB mineral salts have been successfully utilized in a number of applications but it""s uses with experienced weight trained athletes have not been as successful. Int J Sport Nutr Exerc Metab 2001 September; 11(3): 384-96 by Slater et al. and Sports Med 2000 Aug. 30(2): 105-16 by Kreider et al. demonstrates that experienced weight trained athletes do not respond in the same manner to supplemental HMB calcium salts as untrained individuals. Both researchers concluded that there was no alteration in muscle size, fat mass, or strength variables after either 6 weeks or 28 days of oral supplemental HMB calcium salt.
U.S. Pat. No. 5,756,469 by Beale describes a method for the use of pyruvate and/or pyruvyl amino acids in combination with anti-cortisol compounds (HMB) for increasing protein concentration In mammals. Beale states that this combination would have a beneficial impact on the treatment of catabolic conditions associated with diseases such as AIDS and cancer. Beale discloses that this combination was shown to produce a 15 percent increase of lean body mass in healthy rats. This invention represents an improvement in standard nutraceutical preparations due to the combination of pyruvate and/or pyruvyl amino acids and HMB. However this combination would not be efficacious In experienced weight trained athletes due to the economic impracticality of pyruvyl amino acids and the inferior function and bioavailability of orally combining ingredients versus covalently bonded compounds such as HMB amino acid salts.
U.S. Pat. No. 6,031,000 by Nissen describes a method for the use of combining HMB and at least one amino acid. The HMB utilized in this application consists of a sodium salt, a potassium salt, a magnesium salt, a chromium salt, and most preferably a calcium salt, which is the same as previous applications. The amino acids consist of L-isomer essential amino acids and/or a combination of L-glutamine and L-arginine. Nissen states that unlike traditional HMB supplementation resulting in increased muscle mass and deceased fat mass, the combination of HMB and at least one amino acid causes increased muscle mass without decreasing fat mass. This alteration in HMB functionality can be advantageous in animals suffering from body tissue wasting as the result of disease such as AIDS, although this application would not be desirable to most athletes due to the retention of fat mass. The efficacy of such a application with experienced weight trained athletes is not likely due to the well known fact to those skilled in the art that wasting conditions prime the body for weight gain whereas experienced weight trained athletes require potent stimuli in order to produce gains in muscle mass.
U.S. Pat. No. 6,392,092 by Mycoy et al. describes a process for the manufacturing of HMB salts in commercially viable amounts. Mycoy et al. states that HMB is only available in small quantities due to the absence of an efficient synthetic process for large commercial production. The chemical process of this invention utilizes diacetone alcohol to produce free or unbound HMB which is then combined with the appropriate salt. The disclosed chemical procedure is noted to produce a 70% increase in HMB output as compared to standard processes. This process represents an improvement in standard HMB salt production however it does not address production of novel HMB amino acid salts in small or large quantity.
The present invention consists of a process for the synthesis of a HMB amino acid salt and a method for the regulation of athletic function in humans. The method comprises administering to humans an effective amount of a composition consisting of an HMB amino acid salt such as but not limited to HMB-L-Arginine, HMB-L-Glutamine, HMB-Glycylarginine, HMB-Glycylglutamine. This novel combination creates an HMB amino acid salt in which both compounds are combined by a covalent bond.
The chemical synthesis of HMB amino acid salts consists of a three step process and is capable of producing small or very large commercial amount. The process begins with the preparation of an inorganic alkali solution, which is maintained at a temperature of about minus 25 degree Celsius to 50 degree Celsius. The next step involves the addition of an organic alcohol for the formation of a 3-hydroxy-3-methylbutyrate alcohol solution. The final step involves the addition of an amino acid to the solution, which is agitated for about 30 minutes to 3 hours under room temperature in order to produce the finished product consisting of a white crystalline powder. This entire process is novel and unobvious to those skilled in the art since the HMB acid is not separated from the reaction solution, the acid is directly extracted from the reaction solution. This HMB amino acid salt utilizes the peptide carrier system instead of hydrolysis in the gut thereby substantially increasing oral absorption and bioavailability of the intact compound. Once the intact compound enters the blood stream it exerts a dual effect since both HMB and the amino acid contribute to the accretion of lean tissue by different mechanisms. The present invention promotes the development of lean tissue but also decreases fat tissue unlike U.S. Pat. No. 6,031,000 by Nissen, which only promotes lean tissue by orally combining HMB and an amino acid. In fact the covalently bound HMB amino acid salt possess superior results to HMB alone or combined orally with various amino acids and therefore may be utilized as a method for the regulation of athletic function in experienced weight trained athletes.